Clarisense, 1 mg/ml syrup 100 ml

Pharmacotherapeutic group: anti-allergic agent – H1-histamine receptor blocker

ATX code R06AX13

Pharmacological properties

CLARISENS® syrup is an anti-allergic agent, selective blocker of peripheral H1-histamine receptors long-acting.

Pharmacodynamics

It has anti-allergic, antipruritic, antiexudative effects. Inhibits the release of histamine and leukotriene C4 from mast cells. It prevents the development and facilitates the course of allergic reactions. It reduces capillary permeability, prevents the development of tissue edema, relieves spasms of smooth muscles. The antiallergic effect develops quickly – 30 minutes after taking the drug and reaches a maximum after 8-12 hours. The effect lasts for a long time – up to 24 hours. The drug is not addictive and has practically no effect on the central nervous system.

Pharmacokinetics

Loratadine is quickly and completely absorbed in the gastrointestinal tract after oral administration. Time of reaching maximum concentration (TSmax) is 1.3-2.5 hours; eating slows it down by 1 hour. In blood loratadine is almost completely bound to proteins (up to 97%), does not penetrate through the blood-brain barrier, so it has no sedative effect. The maximum concentration of loratadine is reached after 8-12 hours.

In biotransformation the active metabolite is formed – descarboethoxyloratadine with the participation of cytochrome CYP3A4 isoenzymes and to a lesser extent CYP2D6. The elimination half-life is from 3 to 20 hours (on average 8.4 hours). Half-life of active metabolite is 8.8-92 hours (mean 28 hours); in elderly patients, respectively, 6.7-37 hours (mean 18.2 hours) for loratadine and 11-38 hours (17.5 hours) for metabolite. Equilibrium plasma concentrations of loratadine and its metabolite are reached on day 5 of administration.
Loratadine and its metabolites are excreted through the kidneys and intestines.

In patients with chronic renal insufficiency pharmacokinetics do not change. In alcoholic liver damage and in the elderly, the maximum concentration and half-limitation period increase (up to 50% in the elderly and in alcoholic liver damage in proportion to the severity of the disease).

Indications

Active ingredient

Composition

How to take, the dosage

Ingestion, before meals once a day. Adults and children over 12 years of age (with body weight over 30 kg) are prescribed 10 ml of syrup (2 measuring spoons, 10 mg/day). For children from 2 to 12 years of age with body weight less than 30 kg, 5 ml of syrup (1 measuring spoon, 5 mg/day). In case of hepatic insufficiency the drug is taken 10 ml (2 scoops) every other day.

Interaction

CYP3A4 inhibitors (including ketoconazole, erythromycin), CYP3A4 and CYP2D6 inhibitors (cimetidine and others) increase the blood concentration of loratadine.

Microsomal oxidation inducers (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce efficacy.

Special Instructions

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration and quick psychomotor reactions.

Contraindications

High sensitivity to loratadine, period of lactation, children under 2 years.

Side effects

Pregnancy use

Similarities